The TEAD family of transcription factors are regulated by the Hippo tumor suppressor pathway and they act by binding the co-activators YAP and TAZ that drive the transcription of genes involved in cell survival, proliferation, migration, differentiation and resistance.
Researchers from the Beijing Institute of Radiation Medicine have presented the discovery of novel toll-like receptor (TLR)2/1 agonists as potential candidates for the treatment of lung cancer.
Researchers from State University of New Jersey (Rutgers) and Oklahoma State University have published preclinical data for a novel a SARS-CoV-2 papain-like protease (PLpro) inhibitor being developed as an antiviral candidate for the treatment of COVID-19.
Researchers from Shenyang Pharmaceutical University and affiliated organizations have reported the identification of a selective cyclin-dependent kinase 9 (CDK9) inhibitor, CLZX-205, being developed for the treatment of colorectal cancer.
Researchers from the Chinese Academy of Sciences and affiliated organizations discovered a new ubiquitin-specific protease 7 (USP7) inhibitor, YCH-2823, being developed as a potential anticancer agent.
Researchers from Haisco Pharmaceutical Group Co. Ltd. presented the discovery and preclinical characterization of a brain-penetrating BRAF paradox breaker, HSK-42360, being developed for the treatment of BRAF-driven cancers. HSK-42360 proved to be a potent BRAF V600E inhibitor (IC50=5 nM) with selectivity over wild-type BRAF.
Werner syndrome helicase (WRN), which plays important roles in DNA repair and maintenance of genome integrity, has been recently identified as therapeutic target for microsatellite instability (MSI)-H tumors, which have deficiencies in DNA damage repair.
Researchers from Dong-A Socio Holdings Co. Ltd. presented a first-in-class Src homology 2 domain-containing phosphatase 1 (SHP1) allosteric inhibitor, SB-8091, being developed as an anticancer agent.
In tumors with amino acid deprivation, eIF-2α kinase GCN2 is activated and triggers a signaling response to promote cell survival and proliferation. This is important in high metabolically active hematological cancers, such as acute myeloid leukemia (AML).
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